Efforts on targeting the WIN or WBM binding site of WDR5 have led to discovery of several inhibitors that potently and selectively block PPIs between WDR5 and its binding partners.275 However, these WDR5 PPI inhibitors rely on receptor occupancy pharmacology and target only some but not all WDR5 oncogenic functions, exerting poor antiproliferative activity on tumor cells.276. The gene discussed is WDR5; the disease is neoplasm.